|
|
| | 4H-Thiopyran-4-one,tetrahydro-3,5-bis[(4-nitrophenyl)methylene]-1,1-dioxide Basic information |
| Product Name: | 4H-Thiopyran-4-one,tetrahydro-3,5-bis[(4-nitrophenyl)methylene]-1,1-dioxide | | Synonyms: | 4H-Thiopyran-4-one,tetrahydro-3,5-bis[(4-nitrophenyl)methylene]-1,1-dioxide;NSC-144303;Ubiquitin Isopeptidase Inhibitor I;Ubiquitin Isopeptidase Inhibitor I, G5;G5, Ubiquitin Isopeptidase Inhibitor I;Ubiquitin Isopeptidase-IN-G5;Ubiquitin Isopeptidase Inhibitor I, G5 (NSC144303);Ubiquitin Isopeptidase Inhibitor I, G5,Ubiquitin Isopeptidase Inhibitor I, G-5 | | CAS: | 108477-18-5 | | MF: | C19H14N2O7S | | MW: | 414.39 | | EINECS: | | | Product Categories: | | | Mol File: | 108477-18-5.mol | ![4H-Thiopyran-4-one,tetrahydro-3,5-bis[(4-nitrophenyl)methylene]-1,1-dioxide Structure](CAS/20181012/GIF/108477-18-5.gif) |
| | 4H-Thiopyran-4-one,tetrahydro-3,5-bis[(4-nitrophenyl)methylene]-1,1-dioxide Chemical Properties |
| Melting point | 233.5-234.5 °C | | Boiling point | 693.0±55.0 °C(Predicted) | | density | 1.541±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C,unstable in solution, ready to use. | | solubility | ≤15mg/ml in DMSO;1mg/ml in dimethyl formamide | | form | crystalline solid | | color | Light yellow to yellow |
| | 4H-Thiopyran-4-one,tetrahydro-3,5-bis[(4-nitrophenyl)methylene]-1,1-dioxide Usage And Synthesis |
| Description | Ubiquitin isopeptidase inhibitor I induces caspase activation and apoptosis (IC50 = ~1.7 μM) through a Bcl-2-dependent and apoptosome-independent mitochondrial pathway that selectively inhibits ubiquitin isopeptidase activity (IC50 = ~30 μM). It has also been shown to induce necrosis in apoptosis-resistant DKO cells. | | Uses | Ubiquitin Isopeptidase Inhibitor I, G5 is a cell-permeable cross-conjugated unsaturated dienone compound. | | in vitro | ubiquitin isopeptidase inhibitor i targeted the ubiquitinproteasome system via inhibiting the ubiquitin isopeptidases. ubiquitin isopeptidase inhibitor i could induce a rather unique apoptotic pathway, including a bcl-2-dependent but apoptosome-independent mitochondrial pathway with upregulation of the bh3-only protein noxa, stabilization of the inhibitor of apoptosis antagonist smac, but also the involvement of the death receptor pathway. moreover, the treatment of ubiquitin isopeptidase inhibitor i to cell extracts obtained from e1a cells did not inhibit the proteolytic activity of the proteasome, whereas mg-132 potently inhibited the cleavage of the llvy-amc substrate. in addition, noxa induction by ubiquitin isopeptidase inhibitor i could be inhibited by the specific rnai oligos efficiently. when apoptosis was scored, it was found that down-regulation of noxa was able to inhibit but did not suppress apoptosis and caspase activation in response to ubiquitin isopeptidase inhibitor i treatment [1]. | | IC 50 | ~30 μm | | storage | Store at -20°C | | references | [1] e. aleo, c. j. henderson, a. fontanini, et al. identification of new compounds that trigger apoptosome-independent caspase activation and apoptosis. cancer research 66(18), 9235-9244 (2006). |
| | 4H-Thiopyran-4-one,tetrahydro-3,5-bis[(4-nitrophenyl)methylene]-1,1-dioxide Preparation Products And Raw materials |
|